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Pharmacological action of Flonase Nasal Spray
The mechanism of action of
Fluticasone propionate is a substance with a strong anti-inflammatory effect. With intranasal administration, there is no marked systemic action and suppression of the hypothalamic-pituitary-adrenal system.
There was no significant change in the daily area according to the pharmacokinetic curve of serum cortisol after the administration of fluticasone propionate at a dose of 200 μg / day. compared with placebo (ratio: 1.01, 90% CI - CI 0.9 to 1.14).
Fluticasone propionate has an anti-inflammatory effect by interacting with glucocorticosteroid receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils; reduces the production of inflammatory mediators and other biological active substances (histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of an allergic reaction. Fluticasone propionate has a rapid anti-inflammatory effect on the nasal mucosa, and its antiallergic effect appears within 2-4 hours after the first application. Reduces sneezing, itchy nose, runny nose, nasal congestion, sinus discomfort and pressure around nose and eyes. In addition, it relieves eye symptoms associated with allergic rhinitis. A decrease in the severity of symptoms (especially nasal congestion) persists for 24 hours after a single injection of a spray at a dose of 200 μg. Fluticasone propionate improves patients' quality of life, including physical and social activity.
After intranaponic administration of fluticasone propionate at a dose of 200 μg / day. maximum equilibrium plasma concentrations are not quantitatively determined in most patients (less than 0.01 ng / ml). The highest plasma concentration was recorded at 0.017 ng / ml. Direct absorption from the nasal cavity is unlikely due to low water solubility and ingestion of most of the drug. The absolute oral bioavailability is low (less than 1%) as a result of a combination of incomplete absorption from the gastrointestinal tract and active metabolism during the first passage through the liver. The total systemic absorption is thus extremely low.
Fluticasone propionate has a large equilibrium volume of distribution (approximately 318 L). The connection with blood plasma proteins is high (91%).
Fluticasone propionate is rapidly excreted from the systemic circulation, mainly due to metabolism in the liver with the formation of inactive carboxylic acid through the isoenzyme CYP3A4 of the cytochrome P450 system. The metabolism of the swallowed fraction of fluticasone propionate during the first passage through the liver occurs in the same way.
The elimination of fluticasone propionate is linear in the dose range from 250 to 1000 mcg and is characterized by a high plasma clearance (1.1 l / min). The maximum plasma concentration decreases to approximately 98% within 3-4 hours, and only at very low plasma concentrations there was a terminal half-life of 7.8 hours.Renal clearance of fluticasone propionate is negligible (less than 0.2%), and the inactive metabolite is carboxylic acid - less than 5%. Fluticasone propionate and its metabolites are mainly excreted in the bile through the intestines.
Indications of the drug Fluticasone
prevention and treatment of seasonal and perennial allergic rhinitis.
Dosage regimen of Flonase Nasal Spray
To achieve the full therapeutic effect, the drug must be used regularly. The maximum therapeutic effect can be achieved after 3-4 days of therapy.
Adults and children over 12 years of age
For the prevention and treatment of seasonal and year-round allergic rhinitis, 2 injections into each nostril 1 time per day, preferably in the morning (200 mcg per day). In some cases, you can use 2 sprays in each nostril 2 times a day (400 mcg per day) for a short time in order to achieve control over symptoms, after which the dose can be reduced.
The maximum daily dose is 400 mcg (no more than 4 injections into each nostril).
Special patient groups
Usual adult dose.
Children from 4 to 12 years old
For the prevention and treatment of seasonal and year-round allergic rhinitis, 1 injection (50 mcg) in each nostril 1 time a day, preferably in the morning. In some cases, it may be necessary to prescribe 1 spray in each nostril 2 times a day. The maximum daily dose is 200 mcg (no more than 2 injections into each nostril).
Using the inhaler
Before use, gently shake the bottle, take it by placing your index and middle fingers on either side of the tip, and your thumb under the bottom.
When using the drug for the first time or a break in its use for more than 1 week, you should check the operability of the nebulizer: direct the tip away from you, press several times until a small cloud appears from the tip. Next, you need to clear your nose (blow your nose). Close one nostril and insert the tip into the other nostril. Tilt your head slightly forward while continuing to hold the bottle upright. Then you should begin to inhale through the nose and, while continuing to inhale, press once with your fingers to spray the drug. Exhale through your mouth. Repeat the procedure for a second spray into the same nostril, if necessary. Then completely repeat the described procedure, introducing the tip into the other nostril. After use, blot the handpiece with a clean cloth or handkerchief and close it with a cap. The spray should be flushed at least once a week. To do this, carefully remove the tip and rinse it in warm water. Shake off excess water and leave to dry in a warm place. Avoid overheating. Then carefully place the tip back on top of the bottle. Put on the protective cap. If the tip opening is clogged, the tip should be removed as described above and left in warm water for a while. Then rinse under running cold water, dry and put on the bottle again. Do not use a pin or other sharp object to clean the tip hole.
Contraindications to use
hypersensitivity to fluticasone propionate or any other component of the drug;
children under 4 years of age.
concomitant use with strong inhibitors of the CYP3A4 isoenzyme, such as ritonavir and ketoconazole, may cause an increase in plasma concentration of fluticasone propionate;
with simultaneous use with other dosage forms of glucocorticosteroids;
in the presence of infections of the nasal cavity or paranasal sinuses. In this case, infectious diseases of the nose require appropriate treatment, but are not a contraindication to the use of a nasal spray;
after a recent injury to the nose or surgery in the nasal cavity, or in the presence of ulceration of the nasal mucosa.
Application during pregnancy and breastfeeding
Pregnant and lactating women can be prescribed the drug only in cases where the expected benefit to the patient outweighs any possible risk to the fetus or child.
Use in children
For the prevention and treatment of seasonal and year-round allergic rhinitis, 1 injection (50 mcg) in each nostril 1 time per day, preferably in the morning. In some cases, it may be necessary to prescribe 1 spray in each nostril 2 times a day. The maximum daily dose is 200 mcg (no more than 2 injections into each nostril). Contraindicated in children under 4 years of age.
Usual adult dose.
The drug is indicated only for intranasal use.
The nasal spray should not be used continuously for more than 6 months without medical supervision.
With prolonged use, regular monitoring of the function of the adrenal cortex is necessary.
There are reports of the manifestation of systemic effects when using nasal glucocorticosteroids in very high doses for a long time. These effects are much less likely than with the use of oral forms of glucocorticosteroids, and can vary in individual patients, as well as between different glucocorticosteroid drugs.
Potential systemic effects may include Itsenko-Cushing syndrome, adrenal suppression, cataracts, glaucoma, and, in even more rare cases, mental or behavioral disorders, including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression.
In children who received intranasal glucocorticosteroids, a decrease in the growth rate was observed. Therefore, as a maintenance dose in children, the lowest dose should be used that provides adequate control of the symptoms of the disease.
The full effect of fluticasone propionate nasal spray can only appear after a few days of treatment. To achieve the maximum therapeutic effect, it is necessary to adhere to a regular dosage regimen.
Care must be taken when transferring patients from systemic glucocorticosteroid therapy to treatment with fluticasone propionate nasal spray if there is reason to suspect adrenal dysfunction.
In most patients, fluticasone propionate nasal spray relieves symptoms of seasonal allergic rhinitis, but in some cases, when the concentration of allergens in the air is very high, additional therapy may be needed.
For relief of ophthalmic manifestations against the background of successful treatment of seasonal allergic rhinitis, additional therapy may be required.
During post-registration observation, cases of systemic effects of corticosteroids, such as Cushing's syndrome and adrenal suppression, were reported with the combined use of fluticasone propionate and ritonavir. Thus, the concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the possible risk of developing systemic side effects of corticosteroids.
Influence on the ability to drive vehicles, mechanisms
Data on the effect of the drug on the ability to drive vehicles has not been obtained, however, one should take into account the side effects that the drug can cause.
There is no evidence of acute or chronic overdose of fluticasone propionate.
In healthy volunteers, intranasal administration of 2 mg of fluticasone propionate twice a day for 7 days had no effect on the function of the hypothalamic-pituitary-adrenal system (doses 20 times higher than the therapeutic dose). The use of the drug in doses higher than those recommended for a long period of time can lead to temporary suppression of adrenal function.
In these patients, treatment with fluticasone propionate should be continued at doses necessary to control symptoms; recovery of adrenal function takes several days and is monitored by measuring plasma cortisol levels.
Due to the very low plasma concentrations of fluticasone propionate after administration of the nasal spray, clinically significant interactions are unlikely.
Ritonavir (a highly active inhibitor of the coenzyme CYP3A4 of the cytochrome P450 enzyme system) can significantly increase plasma concentrations of fluticasone propionate, resulting in a sharp decrease in serum cortisol levels, systemic side effects, including Cushing's syndrome and suppression of adrenal function, occur.
Inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system cause negligible (erythromycin) or insignificant (ketoconazole) increases in plasma concentrations of fluticasone propionate, which do not entail any noticeable decrease in serum cortisol concentrations. However, caution should be exercised with the combined use of inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system (for example, ketoconazole) and fluticasone propionate due to a possible increase in the plasma concentration of the latter. During post-registration observation, cases of systemic effects of corticosteroids, such as Cushing's syndrome and adrenal suppression, were reported with the combined use of fluticasone propionate and ritonavir. Thus, the concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the possible risk of developing systemic side effects of corticosteroids.
Flonase side effects
Get emergency medical help if you have signs of an allergic reaction to Flonase: hives; Labored breathing; Swelling of the face, lips, tongue, or throat.
Call your doctor at once if you have:
severe or recurrent nosebleeds;
Noisy breathing, runny nose, or crusting around your nostrils;
Redness, sores, or white patches in your mouth or throat;
Fever, chills, weakness, nausea, vomiting, flu symptoms;
Any wound that won't heal; or
blurred vision, eye pain, or vision of halos around lights.
Common side effects of Flonase may include: Minor
nosebleeds, burning or itching in the nose;
Sores or white patches in or around the nose;
Cough, shortness of breath;
Headache, back pain;
Sinus pain, sore throat, fever; or